Triethyl phosphite → N-cyclopropyl-5-(diethylphosphonomethyl)-1-{4-[(ethylamino)carbonyl]phenyl}-1H-1,2,3-triazole-4-carboxamide

Participants

Reaction Conditions

Reaction Steps

5-(Bromomethyl)-N-cyclopropyl-1-{4-[(ethylamino)carbonyl]phenyl}-1H-1,2,3-triazole-4-carboxamide (890 mg) obtained in Example 321a) was dissolved in triethyl phosphite (2 ml), and the mixture was stirred at 120° C. for 3 days. An excess amount of triethyl phosphite was evaporated under reduced pressure, and the obtained residue was purified by silica gel column (ethyl acetate to ethyl acetate/methanol=4/1) to give the title compound as a colorless oil (640 mg).

Provenance & Evidence